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GABBR1 / GABA B Receptor 1
gamma-aminobutyric acid (GABA) B receptor, 1
Component of a heterodimeric G-protein coupled receptor for GABA, formed by GABBR1 and GABBR2. Within the heterodimeric GABA receptor, only GABBR1 seems to bind agonists, while GABBR2 mediates coupling to G proteins. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase, stimulates phospholipase A2, activates potassium channels, inactivates voltage-dependent calcium-channels and modulates inositol phospholipid hydrolysis. Calcium is required for high affinity binding to GABA. Plays a critical role in the fine-tuning of inhibitory synaptic transmission. Pre-synaptic GABA receptor inhibits neurotransmitter release by down-regulating high-voltage activated calcium channels, whereas postsynaptic GABA receptor decreases neuronal excitability by activating a prominent inwardly rectifying potassium (Kir) conductance that underlies the late inhibitory postsynaptic potentials. Not only implicated in synaptic inhibition but also in hippocampal long-term potentiation, slow wave sleep, muscle relaxation and antinociception. Activated by (-)-baclofen, cgp27492 and blocked by phaclofen.Isoform 1E may regulate the formation of functional GABBR1/GABBR2 heterodimers by competing for GABBR2 binding. This could explain the observation that certain small molecule ligands exhibit differential affinity for central versus peripheral sites.
| Gene Name: | gamma-aminobutyric acid (GABA) B receptor, 1 |
| Family/Subfamily: | GPCR , GABA(B) |
| Synonyms: | GABBR1, DJ271M21.1.1, DJ271M21.1.2, GABA(B) receptor, Gaba-b-r1a, GABA-BR1, Gaba-br1a receptor, GABAB, subunit 1c, GABAB1, GABA-B receptor 1, Gaba-b1, Gababr1 receptor, GPRC3A, Gabab-receptor subunit 1a, GABABR1, GABBR1-3, GBR1, HGB1a, GABA-B-R1, GB1 |
| Target Sequences: | NM_001470 NP_001461.1 Q9UBS5 |
Publications (2)
![GABBR1 / GABA B Receptor 1 Antibody - Immunofluorescence of monoclonal antibody to GABBR1 on HeLa cell. [antibody concentration 10 ug/ml]](https://lsbio-7d62.kxcdn.com/image2/gabbr1-gaba-b-receptor-1-antibody-clone-2d7-ls-c197262/144948_4846510.jpg)
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